312904-86-2Relevant academic research and scientific papers
Development of a scaleable synthesis of a 3-aminopyrazinone acetamide thrombin inhibitor
Ashwood, Michael S.,Alabaster, Ramon J.,Cottrell, Ian F.,Cowden, Cameron J.,Davies, Antony J.,Dolling, Ulf H.,Emerson, Khateeta M.,Gibb, Andrew D.,Hands, David,Wallace, Debra J.,Wilson, Robert D.
, p. 192 - 200 (2013/09/04)
A scaleable route to 2-{3-[(2,2-difluoro-2-(2-pyridyl)ethyl)-animo]-6- chloro-2-oxohydropyrazinyl}-N-(3-fluoro(2-pyridyl))-methyl]acetamide 1 is described in which various scaleup issues were addressed to provide a safe, efficient, and robust route for th
Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines
Burgey, Christopher S.,Robinson, Kyle A.,Lyle, Terry A.,Sanderson, Philip E. J.,Lewis, S. Dale,Lucas, Bobby J.,Krueger, Julie A.,Singh, Rominder,Miller-Stein, Cynthia,White, Rebecca B.,Wong, Bradley,Lyle, Elizabeth A.,Williams, Peter D.,Coburn, Craig A.,Dorsey, Bruce D.,Barrow, James C.,Stranieri, Maria T.,Holahan, Marie A.,Sitko, Gary R.,Cook, Jacquelynn J.,McMasters, Daniel R.,McDonough, Colleen M.,Sanders, William M.,Wallace, Audrey A.,Clayton, Franklin C.,Bohn, Dennis,Leonard, Yvonne M.,Detwiler Jr., Theodore J.,Lynch Jr., Joseph J.,Yan, Youwei,Chen, Zhongguo,Kuo, Lawrence,Gardell, Stephen J.,Shafer, Jules A.,Vacca, Joseph P.
, p. 461 - 473 (2007/10/03)
Recent efforts in the field of thrombin inhibitor research have focused on the identification of compounds with good oral bioavailability and pharmacokinetics. In this manuscript we describe a metabolism-based approach to the optimization of the 3-(2-phen
Process for making a thrombin inhibitor
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, (2008/06/13)
The invention is a process for preparing 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide which comprises coupling with 2-aminomethyl-3-fluoropyridine dihydrochloric acid salt in the presence of a coupling reagent and a base to form 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide.
